Fenfluramine HCl – (404-82-0)

Fenfluramine is a serotonergic medication primarily used for the treatment of seizures associated with Dravet syndrome and Lennox-Gastaut syndrome in patients aged two years and older. Initially developed in the early 1960s as an appetite suppressant for obesity, fenfluramine was withdrawn from the market in the late 1990s due to cardiovascular toxicity concerns, including heart valve disease and pulmonary arterial hypertension.

Fenfluramine acts as a serotonin and norepinephrine releasing agent, agonist of the serotonin 5-HT2 receptors, and sigma σ1 receptor positive modulator. Its exact mechanism of action in treating seizures is not fully understood but is believed to involve increased activation of certain serotonin receptors and the sigma σ1 receptor. The drug is known to increase extracellular serotonin levels, which can lead to a feeling of fullness and reduced appetite, making it effective for weight loss but also contributing to its side effects.

In clinical studies, fenfluramine has demonstrated a significant reduction in seizure frequency, particularly in generalized tonic-clonic seizures, which are a key risk factor for sudden unexpected death in epilepsy (SUDEP). It has also shown improvements in everyday executive functioning and potential benefits in reducing SUDEP risk.

Despite its effectiveness, fenfluramine’s use is accompanied by several precautions and contraindications. It should be used with caution in patients taking CNS depressant drugs and is contraindicated in those with severe hypertension, glaucoma, symptomatic cardiovascular disease, and known hypersensitivity to fenfluramine or other sympathomimetic amines.

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Sources:

https://en.wikipedia.org/wiki/Fenfluramine
https://pubchem.ncbi.nlm.nih.gov/compound/91452
https://www.thelancet.com/journals/lancet/article/PIIS0140-6736(19)32500-0/abstract
https://www.sciencedirect.com/science/article/abs/pii/S0140673619325000